Repotrectinib (TPX-0005)

Catalog No.S8583

Repotrectinib (TPX-0005) Chemical Structure

Molecular Weight(MW): 355.37

TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).

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Biological Activity

Description TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).
Targets
WT ALK [1]
(Cell-free assay)		 ALK(L1196M) [1]
(Cell-free assay)		 ALK(G1202R) [1]
(Cell-free assay)		 Src [1]
(Cell-free assay)
1.01 nM 1.08 nM 1.26 nM 5.3 nM
In vitro

TPX-0005 is an orally available and potent ATP-competitive inhibitor against ALK, ROS1, TRKA, TRKB and TRKC recombinant kinases and their corresponding clinical resistant mutants. TPX-0005 demonstrates potent anti-proliferative activity in the range of sub-nanomolar to low nanomolar in a number of human cancer cell lines and engineered stable cell lines expressing the targeted oncogenes or their solvent front mutants, accompanied by inhibition of target phosphorylation and concomitant inactivation of downstream effectors such as ERK, AKT and STAT3[2]. TPX-0005 inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib. TPX-0005 is able to not only inhibit the wild-type and a broad spectrum of mutant ALKs, but also overcome primary resistance and suppress metastatic features by inhibiting SRC[1].

Assay
Methods Test Index PMID
Western blot
pEGFR / pERK / pAKT / pSTAT3 / pPaxillin / Pyap1 / cleaved caspase-3; 

PubMed: 29433983     


Extracts from the PC9 cell line treated with gefitinib (0.05 μM), TPX-0005 (1 μM), or the double combination for 24 h, were analyzed using the indicated antibodies. Similar results were obtained in three independent experiments.

29433983
Immunofluorescence
pSTAT3(Y705) / STAT3 ; 

PubMed: 29433983     


Representative immunofluorescence images showing total STAT3 and phospho-STAT3 expression and localization (green) in control, gefitinib, TPX-0005 and gefitinib plus TPX-0005 treated PC9 cells. Cell nuclei were stained with DAPI (blue). Right: expression levels and nuclear translocation of phospho-STAT3 were quantified using an ImageStreamX imaging flow cytometer. 

29433983
In vivo In patient derived xenograft tumor models, TPX-0005 treatment results in significant regression of tumors harboring the oncogenic ALK, ROS1 and TRKC fusions. Moreover, in a series of mouse xenograft tumor models, TPX-0005 exhibits marked anti-tumor activity not only in tumors harboring the wildtype oncogenic targets but also in tumors harboring the oncogenes with the solvent front mutations via inhibition of the target phosphorylation[2].

Protocol

Solubility (25°C)

In vitro DMSO 70 mg/mL (196.97 mM)
Ethanol 10 mg/mL (28.13 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 355.37
Formula

C18H18FN5O2
CAS No. 1802220-02-5
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03093116 Recruiting Locally Advanced Solid Tumors|Metastatic Solid Tumors|Non Hodgkin Lymphoma TP Therapeutics Inc. February 27 2017 Phase 1|Phase 2
NCT03093116 Recruiting Locally Advanced Solid Tumors|Metastatic Solid Tumors|Non Hodgkin Lymphoma TP Therapeutics Inc. February 27 2017 Phase 1|Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID